Pipeline

MY004567, a Class 1 new drug independently developed by Createrna, is an interleukin receptor-associated kinase-4 (IRAK4) inhibitor, intended to be developed for rheumatoid arthritis and other clinical indications. Received clinical trial approval from NMPA on June 18 and FDA on August 6, 2021 respectively (FDA informed by email on August 6 that there were no defects causing clinical-Hold, provided Study May Proceed Letter on August 12), and has now completed Phase I clinical trial.

IRAK-4 is involved in innate immune regulation, primarily responsible for transduction of signals from TLR and members of the IL-1β receptor family. IRAK4 plays a key role in many important signaling pathways such as NF-κB and MAPK, so it has a broad clinical application prospect.

MY009212A is a Class 1 new drug independently developed by Createrna. It is a vascular non-inflammatory protein-1 (Vanin-1 or VNN1) inhibitor, intended to be developed for clinical indications such as inflammatory bowel disease (IBD). It received clinical trial approval from NMPA on April 18, 2022, and has basically completed phase I clinical trials.

Currently, there are no vasonon-inflammatory protein-1 (VNN1) inhibitors entering the clinical stage in the world, and MY009212A is the first VNN1 inhibitor entering clinical trials in the world, providing a new drug choice for clinical IBD treatment.

QR052107B tablet is a class 1 new drug independently developed by Createrna for the treatment of refractory or unknown chronic cough. It was approved for clinical trials by NMPA on June 10, 2021, and has completed phase I clinical trials at present.

Chronic cough refers to the cough lasting for more than 8 weeks. According to the relevant literature, the prevalence of slow cough is 9.6% worldwide, and about 600 million people are suffering from this disease. The continuous existence of cough not only affects the daily life of patients, but also brings huge burden to patients' psychological and social. However, currently available drugs for chronic cough are limited, and the clinical treatment effect is not good, and the existing therapeutic means are difficult to meet the treatment needs of this disease.

QR052107B tablet is the latest generation of highly selective P2X3 receptor antagonist, which is the first class 1 new drug that can be taken orally once a day into clinic in China. It can completely avoid adverse reactions related to taste disorders, and is expected to achieve better efficacy and compliance, meeting the actual needs of patients with slow cough.

QR056251 capsules are designed to be used in the treatment of idiopathic pulmonary fibrosis (IPF). Received FDA approval for clinical trials on July 14, 2022.

At present, only pirfenidone and Nidanib have been marketed in the world for IPF treatment, and their efficacy and safety are insufficient, and the therapeutic effect is limited.

QR056251 as a new generation of ROCK1/2 inhibitor, bleomycin-induced rat pulmonary fibrosis model has better efficacy at lower dose and exposure concentration. Preclinical studies have shown that QR056251 has better efficacy and higher safety window than marketed drug Nidanib, and its preclinical safety is better than marketed ROCK2 inhibitor, which has the potential to become the best in-class drug. It is expected to provide safer and more effective therapeutic drugs for IPF patients and improve the choice of clinical drugs for patients.

MY008211A is A Class 1 new drug independently developed by Createrna. It is a Complement factor B (CFB) inhibitor intended to be developed for clinical indications such as paroxysmal sleep hemoglobinuria (PNH) and immunoglobulin A nephropathy (IgA nephropathy). It received clinical trial approval from NMPA on April 18, 2022, and has basically completed phase I clinical trials.

CFB is a trypsin-like serine protease that circulates in the human blood as a potential proenzyme. CFB inhibitors inhibit C3 invertase and C5 invertase activities, and prevent MAC formation and intravascular hemolysis. At the same time, the positive feedback amplification mechanism is inhibited to prevent extravascular hemolysis and breakthrough hemolysis. Studies on CFB inhibitors have shown that CFB inhibitors can significantly improve hemolysis in PNH patients with no significant improvement in the treatment of C5 monoclonal antibody Eulizumab, and have a good effect on both intravascular and intravascular hemolysis. The results of in vitro hemolysis test of red blood cells of PNH patients carried out by the company in cooperation with Wuhan Tongji Medical College showed that MY008211A significantly improved the hemolysis of red blood cells in patients.

QR01019 potassium salt is a Class 2.1 new drug independently developed by Createrna, which is the precursor of Azisartan. The core compound patents are authorized by China and the United States respectively.

This product is the company's first improved new drug for the treatment of essential hypertension, which was reported in both China and the United States. In 2018, it successfully obtained the clinical approval of China, which is an important milestone in the transformation of Createrna into an innovative international pharmaceutical enterprise. Phase I clinical trials of this product have been completed in China, and the results show that this product has good safety and bioequivalence compared with Azisartan ester tablets which have been marketed abroad. To file an IND with FDA in March 2023.

QR12000 compound tablet is an angiotensin II receptor-enkeenase dual inhibitor independently developed by Createrna. It is composed of QR01019 potassium salt with intellectual property rights and Shakuba triammonium salt, which is mainly used for hypertension and chronic heart failure. It was approved for clinical trial by NMPA on November 13, 2020.

At present, only Novartis' Nohintol has been marketed in China with the same target. QR12000 compound tablets have great development potential, which is expected to provide a new choice for the treatment of hypertension and chronic heart failure, and bring new hope to the majority of patients with hypertension and chronic heart failure.

The results of non-clinical studies of QR12000 compound tablets showed that the synergistic effect of QR01019 potassium salt and Shakuba Qu ammonium salt on blood pressure reduction was significantly stronger than that of QR01019 potassium salt and Shakuba Qu ammonium salt, as well as that of nohintal. At the same time, it could reduce the degree and incidence of myocardial thickening and significantly improve cardiac function, and it was dose-dependent. Phase I clinical trial results showed good safety. Phase II trials are underway for hypertension indications.